Oxiconazole (Monograph)

Brand name: Oxistat
Drug class: Azoles
ATC class: G01AF17
VA class: DE102
Chemical name: 1-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-yl)ethanone (Z)-O-[(2,4-Dichlorophenyl)methyl]oxime mononitrate
Molecular formula: C₁₈H₁₃C₁₄N₃O•HNO₃
CAS number: 64211-46-7

Introduction

Antifungal; azole (imidazole derivative).

Uses for Oxiconazole

Dermatophytoses

Treatment of tinea corporis (body ringworm) and tinea cruris (jock itch) caused by Epidermophyton floccosum, Microsporum canis^{† [off-label]}, M. gypseum^{† [off-label]}, Trichophyton mentagrophytes, T. rubrum, or T. verrucosum^{† [off-label]}.

Treatment of tinea pedis or tinea manuum^{† [off-label]} caused by E. floccosum, M. canis^{† [off-label]}, M. gypseum^†, T. mentagrophytes, T. rubrum, or T. verrucosum^†.

Topical antifungals usually effective for treatment of uncomplicated tinea corporis or tinea cruris. An oral antifungal may be necessary when tinea corporis or tinea cruris is extensive, dermatophyte folliculitis is present, infection is chronic or does not respond to topical therapy, or patient is immunocompromised because of coexisting disease or concomitant therapy.

Topical antifungals usually effective for treatment of uncomplicated tinea pedis or tinea manuum. An oral antifungal may be necessary for treatment of hyperkeratotic areas on the palms and soles, for chronic moccasin-type (dry-type) tinea pedis, and for tinea unguium (fingernail or toenail dermatophyte infections, onychomycosis).

Pityriasis (Tinea) Versicolor

Treatment of pityriasis (tinea) versicolor caused by Malassezia furfur (Pityrosporum orbiculare or P. ovale).

Topical antifungals usually effective; an oral antifungal (with or without a topical antifungal) may be necessary in patients who have extensive or severe infections or failed to respond to or have frequent relapses with topical therapy.

Cutaneous Candidiasis

Treatment of cutaneous candidiasis^† caused by Candida albicans or C. tropicalis.

Oxiconazole Dosage and Administration

Administration

Topical Administration

Apply topically to the skin as a 1% cream or lotion.

Do not apply to the eye or administer intravaginally.

Avoid contact with the nose, mouth, and other mucous membranes.

Do not use with occlusive dressings or wrappings, unless otherwise directed by clinician.

Shake lotion well before using.

Apply a sufficient amount of cream or lotion; rub gently into affected area and immediately surrounding healthy skin.

Dosage

Available as oxiconazole nitrate; dosage expressed in terms of oxiconazole.

Pediatric Patients

Dermatophytoses

Tinea Corporis or Tinea Cruris

Topical

Apply 1% cream once or twice daily for 2 weeks.

If clinical improvement does not occur after treatment, reevaluate diagnosis.

Tinea Pedis

Topical

Apply 1% cream once or twice daily for 1 month.

If clinical improvement does not occur after treatment, reevaluate diagnosis.

Pityriasis (Tinea) Versicolor

Topical

Apply 1% cream once daily for 2 weeks.

If clinical improvement does not occur after treatment, reevaluate diagnosis.

Normalization of hyper- or hypopigmented patches on trunk, neck, arms, and upper thighs is variable and may take months.

Adults

Dermatophytoses

Tinea Corporis or Tinea Cruris

Topical

Apply 1% cream or lotion once or twice daily for 2 weeks.

If clinical improvement does not occur after treatment, reevaluate diagnosis.

Tinea Pedis

Topical

Apply 1% cream or lotion once or twice daily for 1 month.

If clinical improvement does not occur after treatment, reevaluate diagnosis.

Pityriasis (Tinea) Versicolor

Topical

Apply 1% cream once daily for 2 weeks.

If clinical improvement does not occur after treatment, reevaluate diagnosis.

Normalization of hyper- or hypopigmented patches on trunk, neck, arms, and upper thighs is variable and may take months.

Special Populations

No special population dosage recommendations at this time.

Cautions for Oxiconazole

Contraindications

Known hypersensitivity to oxiconazole or any ingredient in the formulation.

Warnings/Precautions

Warnings

Application Precautions

For external use only. Use only for topical application to the skin; not for ophthalmic or intravaginal use.

Sensitivity Reactions

Hypersensitivity Reactions

Contact dermatitis reported following topical application of oxiconazole or other imidazole-derivative azole antifungals.

If irritation or sensitivity occurs, discontinue the drug and initiate appropriate therapy.

Possible cross-sensitization among the imidazoles.

Specific Populations

Pregnancy

Category B.

Lactation

Distributed into milk; caution if used in nursing women.

Pediatric Use

Cream may be used in pediatric patients; has been used in children ≤10 years of age without unusual adverse effect.

Safety and efficacy of lotion not established in children.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether safety and efficacy differ from that in younger adults.

Available data to date indicate no difference in safety compared with younger adults; dosage adjustment not recommended.

Common Adverse Effects

Pruritus, burning, irritation, stinging.

Drug Interactions

No formal drug interaction studies to date.

Oxiconazole Pharmacokinetics

Absorption

Bioavailability

Only low concentrations absorbed systemically following topical application to skin.

Distribution

Extent

Topical application to skin results in highest concentrations in epidermis and lower concentrations in upper and deeper corneum. In vitro on animal skin, oxiconazole 1% cream was retained in the horny layer of the epidermis for up to 96 hours after topical application.

Distributed into milk.

Not known whether systemically absorbed oxiconazole crosses the placenta.

Elimination

Elimination Route

Systemically absorbed drug excreted in urine (<0.3% of topical dose).

Stability

Storage

Topical

Cream and Lotion

15–30C; cream is stable for 24 months after the date of manufacture.

Actions and Spectrum

• Imidazole-derivative azole antifungal.

• Usually fungistatic; may be fungicidal at high concentrations or against very susceptible organisms.

• Presumably exerts its antifungal activity by altering cellular membranes, resulting in increased membrane permeability, secondary metabolic effects, and growth inhibition. Fungistatic activity may result from interference with ergosterol synthesis.

• Spectrum of antifungal activity includes many fungi, including yeasts and dermatophytes. Also has in vitro activity against some gram-positive bacteria.

• Dermatophytes: Active in vitro against Epidermophyton floccosum, Microsporum audouinii, M. canis, M. gypseum, Trichophyton mentagrophytes, T. rubrum, T. tonsurans, and T. violaceum.

• Candida: Active in vitro against Candida albicans, C. glabrata (Torulopsis glabrata), C. guilliermondii, C. krusei, C. parapsilosis, and C. tropicalis.

• Other fungi: Active in vitro against Malassezia furfur (Pityrosporum orbiculare). Also active in vitro against Aspergillus flavus, A. fumigatus, A. nidulans, A. niger, Cryptococcus neoformans, Epidermophyton floccosum, Exophiala werneckii, Petriellidium boydii, and Sporothrix schenkii.

• Bacteria: Active in vitro against Actinomadura madurae, Corynebacterium minutissimum, Nocardia asteroides, N. brasiliensis, and Streptomyces somaliensis.

• Cross-resistance can occur among the azole antifungals. Some C. albicans resistant to ketoconazole show cross-resistance to oxiconazole and other imidazole-derivative antifungals as well as to triazole derivatives.

• Some strains of M. furfur (Pityrosporum orbiculare) resistant to oxiconazole in vitro are cross-resistant to econazole.

Advice to Patients

• Importance of completing full course of treatment, even if symptoms improve.

• Importance of contacting clinician if skin condition worsens during therapy or if improvement does not occur after completing full course of therapy.

• Importance of applying to affected areas as directed and avoiding contact with eyes, nose, mouth, or mucous membranes.

• Importance of not using occlusive dressings, unless otherwise directed by clinician.

• Importance of washing hands after applying oxiconazole.

• Importance of discontinuing use and contacting clinician if treated area becomes irritated (e.g., itching, burning, blistering, swelling, oozing).

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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